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1. 发明授权

US5189027A 2-substituted adenosine derivatives and pharmaceutical compositions for circulatory diseases 失效
标题翻译： 2-取代的腺苷衍生物和用于循环疾病的药物组合物
公开(公告)号：US5189027A
公开(公告)日：1993-02-23
申请号：US799071
申请日：1991-11-27
申请人： Takanori Miyashita , Toichi Abiru , Yohko Watanabe , Toyofumi Yamaguchi , Akira Matsuda
发明人： Takanori Miyashita , Toichi Abiru , Yohko Watanabe , Toyofumi Yamaguchi , Akira Matsuda
IPC分类号： C07H19/16
CPC分类号： C07H19/16 , Y02P20/55
摘要： Disclosed herein are a novel 2-substituted adenosine derivative having the following formula [I] ##STR1## wherein R represents a hydrogen atom or a hydroxyl group, m is an integer of 2 to 7, n is 0 or an integer of 1 to 3, and R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each independently represent a hydrogen atom, a hydroxy protective group or a phosphoric acid residue, and salts thereof.The above compounds are excellent in a circulation ameliorating effect such as a vasodepressor activity, and have high selectivity for A.sub.2 receptors, but cause less undesirable side effects such as a suppresssive effect on the heart. They are therefore effective when used in pharmaceutical compositions for circulatory diseases.

2. 发明授权

US5459254A Process for preparing synthetic intermediates of 2-alkynyladenosines and 2-alkynyladenosines 失效
标题翻译：制备2-炔基腺苷和2-炔基腺苷合成中间体的方法
公开(公告)号：US5459254A
公开(公告)日：1995-10-17
申请号：US149943
申请日：1993-11-10
申请人： Toyofumi Yamaguchi , Takanori Miyashita , Shinji Sakata , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
发明人： Toyofumi Yamaguchi , Takanori Miyashita , Shinji Sakata , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
IPC分类号： C07H19/16 , C07H19/067
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## [I] A=a leaving group, [II] A=NH.sub.2,[V] A=NHR.sup.4,wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
摘要翻译：本发明涉及可用作2-炔基腺苷合成中间体的下式[I]表示的新型化合物。本发明还涉及该化合物的制备方法和通过该化合物制备2-炔基腺苷[Ⅳ]的方法。此外，本发明涉及具有优异的储存稳定性的由下式[V]表示的2-炔基腺苷衍生物，以及以该衍生物的形式存储2-炔基腺苷的方法。 [I] A =离去基团，[II] A = NH 2，[V] A = NHR 4，其中R 1至R 4表示氢原子或保护基，n表示1至15的整数， R1至R4同时不表示氢原子。

3. 发明授权

US5283327A Tri-O-acetyl-2-alkynyladenosines 失效
标题翻译：三-O-乙酰基-2- alkynyladenosines
公开(公告)号：US5283327A
公开(公告)日：1994-02-01
申请号：US655354
申请日：1991-04-17
申请人： Toyofumi Yamaguchi , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
发明人： Toyofumi Yamaguchi , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
IPC分类号： C07H19/16 , C07H19/167
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
摘要翻译： PCT No.PCT / JP90 / 00807 Sec。 371日期：1991年4月17日 102（e）中的日期1991年4月17日提交的PCT 1990年6月20日的PCT公布。出版物WO90 / 15812 PCT 日本1990年12月27日。本发明涉及可用作2-炔基腺苷合成中间体的下式（I）表示的新化合物。本发明还涉及该化合物的制备方法和通过该化合物制备2-炔基腺苷（Ⅳ）的方法。此外，本发明涉及具有优异储存稳定性的下式（V）表示的2-链炔基腺苷衍生物，以及以该衍生物的形式存储2-炔基腺苷的方法。（*化学结构*）（*化学结构*）其中R1至R4表示氢原子或保护基，n表示1至15的整数，条件是R1至R4同时不表示氢原子。

4. 发明授权

US5270304A Therapeutic 2-alkynyl adenosine agent for ischemic diseases of the heart or brain 失效
标题翻译：用于心脏或脑部缺血性疾病的治疗性2-炔基腺苷
公开(公告)号：US5270304A
公开(公告)日：1993-12-14
申请号：US700156
申请日：1991-05-15
申请人： Kentaro Kogi , Toichi Abiru , Toyofumi Yamaguchi
发明人： Kentaro Kogi , Toichi Abiru , Toyofumi Yamaguchi
IPC分类号： C07H19/16 , A61K31/52
CPC分类号： A61K31/70 , C07H19/16
摘要： The present invention concerns a therapeutic-prophylactic agent for ischemic diseases of the heart or brain, comprising as an active ingredient a 2-alkynyladenosine represented by the following formula: ##STR1## wherein n represents an integer of from 2 to 15.
摘要翻译： PCT No.PCT / JP89 / 01158 Sec。 371日期1991年5月15日 102（e）日期1991年5月15日PCT提交1989年11月15日PCT公布。出版物WO90 / 05526 日期：1990年5月31日本发明涉及心脏或脑的缺血性疾病的治疗性预防剂，其包含作为活性成分的下式表示的2-炔基腺苷：其中n表示整数从2到15。

5. 发明授权

US5939543A Stable solid 2-octynyl adenosine and process for producing the same 失效
标题翻译：稳定的固体2-辛炔基腺苷及其制备方法
公开(公告)号：US5939543A
公开(公告)日：1999-08-17
申请号：US833718
申请日：1992-02-11
申请人： Manami Morozumi , Masao Kumagai , Toyofumi Yamaguchi
发明人： Manami Morozumi , Masao Kumagai , Toyofumi Yamaguchi
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P9/12 , C07H19/16 , C07H19/167
CPC分类号： C07H19/16
摘要： The present invention provides two kinds of solid 2-octynyl adenosine products with novel properties which are stabilized with respect to temperature or temperature and humidity, one being solid 2-octynyl adenosine having a moisture content of not more than 3%, and the other being solid 2-octynyl adenosine deposited from an anhydrous alcoholic solution or hydrous alcoholic solution of 2-octynyl adenosine, said hydrous alcoholic solution having a water content of less than 1%.
摘要翻译：本发明提供两种具有新的性质的固体2-辛炔基腺苷产品，它们相对于温度或温度和湿度是稳定的，一种是水分含量不大于3％的固体2-辛炔基腺苷，另一种是由2-乙炔基腺苷的无水醇溶液或含水醇溶液沉积固体2-辛炔基腺苷，所述含水醇溶液的含水量小于1％。

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